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Gonadal hormones

Gonadal hormones. The three sex hormones are estrogen, progesterone and testosterone. Estrogen. Natural estrogens : Estradiol, Estrone and Estriol. Synthetic Steroidal : Ethinyl Estradiol, Mestranol. Synthetic Non-steroidal : Diethylstilbestrol, Dienestrol. Estrogen.

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Gonadal hormones

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  1. Gonadal hormones The three sex hormones are estrogen, progesterone and testosterone

  2. Estrogen • Natural estrogens : Estradiol, Estrone and Estriol. • Synthetic Steroidal: Ethinyl Estradiol, Mestranol. • Synthetic Non-steroidal : Diethylstilbestrol, Dienestrol.

  3. Estrogen Physiological actions of estrogen : • Estrogens ↑the synthesis of II, VII, IX, X, fibrinogen and ↓ anti-thrombin. • Estrogen – continuous exposure leads to hyperplasia of endometrium. • It decrease the LDL and increase HDL.

  4. Estrogen Physiological actions of estrogens : • Estrogen sensitizes the myometrium to oxytocin at term and facilitates labor. • Estrogen decrease the resorption of bone.

  5. Estrogen Indications of Estrogens : • Hypogonadism in girls. • Hormonal replacement therapy • Contraception • Osteoporosis • Prostate carcinoma • Turner's syndrome (Gonadal dysgenesis).

  6. Estrogen Adverse Effects : • Gall stones and pulmonary embolism. • ↑ the risk of endometrial and breast cancer. • DES during pregnancy increase vaginal adenocarcinoma in female offspring.

  7. Selective Estrogen Receptor Modulator(SERM) Clomiphene: • It acts by inhibiting the action of estrogen on the hypothalamus / pituitary gland. • It ↓ the negative feedback of estrogen on hypothalamus / pituitary and ↑FSH / LH secretion. • Used as ovulation inducing drug. • Adverse effects – multiple pregnancy.

  8. Selective Estrogen Receptor Modulator(SERM) Tamoxifen : It is a partial agonist at estrogen receptor. • Agonist on bone and lipid metabolism. • Antagonist on breast. • Used in advanced breast cancer in postmenopausal women. • Partial agonist on endometrium can cause endometrial cancer.

  9. Selective Estrogen Receptor Modulator (SERM) Raloxifene: • Agonist on bone and lipid metabolism. • Antagonist on endometrium and breast. • Does not cause endometrial cancer. • It is used for the prevention of post menopausal osteoporosis.

  10. Aromatase inhibitor Anastrozole is a selective inhibitor of aromatase and thus ↓estrogen synthesis. • Used in post menopausal breast cancer resistant to tamoxifen. Anastrozole

  11. Progestins • First generation: Norethindrone, Ethynodiol diacetate. • Second generation: Levonorgestrel,Norgestrel. • Third generation: Desogestrel, Norgestimate. • Fourth generation: Drospirenone.

  12. Progestins Clinical uses : • Hormonal replacement therapy • Contraception Adverse effects : • Breakthrough bleeding • Hirsutism and acne (androgenic) • Abnormal lipid and glucose levels.

  13. Antiprogestins Mifepristone: • It is a progesterone receptor antagonist. It is also a glucocorticoid receptor antagonist. • If mifepristone is taken shortly after intercourse, it prevents pregnancy. • Mifepristone is widely used to terminate early pregnancy.

  14. Hormonal contraceptives They are of two types : • Estrogen and Progestin • Progestin Only These exert the contraceptive effect mainly through selective inhibition of gonadotropin release from the pituitary, especially midcycle LH surge.

  15. Hormonal contraceptives Contents of oral contraceptives: • Estrogen:Ethinly estradiol (EE), Mestranol • Progesterone: Norethindrone, Norgestrel, Levonorgestrel, Desogestrel, Drospirenone.

  16. Hormonal contraceptives Oral contraceptives are classified as monophasic, biphasic and triphasic depending upon the estrogen and progestin content. • Monophasic They contain same amount of estrogen and progestin throughout the cycle. • Biphasic and Triphasic These contain variable amount of estrogen and progesterone in phases.

  17. Hormonal contraceptives

  18. Hormonal contraceptives Benefits of oral contraceptives : • Decrease risk of endometrial and ovarian cancer. • Decrease risk of endometriosis. • Reduced incidence of pelvic inflammatory disease. • Decrease osteoporosis.

  19. Hormonal contraceptives Progesterone only: Mini pills : • Norethindrone (Nor-QD)orally. • Levonorgesterol implanted under the skin. • Medroxyprogesterone depot injection. • IUD of progesterone.

  20. Hormonal contraceptives Progesterone Only: • MDPA (Depo-Provera) depot injection will provide effective contraception for upto 3 months. • Levonorgestrel subcutaneous implant are effective for ~ 5 yrs. • They are suited for women who smoke and estrogen contraindicated. • Failure rates are high.

  21. Hormonal contraceptives Postcoital contraception :"morning-after pill" • Oral levonorgestrel: within 120 hours for best results. • Estrogens and Progestins : It is started within 72 hrs for best results. • Mifepristone is effective as postcoital contraception along with misopristol (PGE1).

  22. Androgens Testosterone • Testosterone is responsible for normal development of male fetus, changes in male at puberty and also to maintain fertility and libido. • Testosterone and related androgens are produced by the testes, adrenal gland and ovary.

  23. Androgens Testosterone

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  25. Androgens Testosterone • It is given i.m or transdermally to avoid extensive hepatic metabolism. • Testosterone cypionate is available for intramuscular administration. • Methyltestosterone is active orally and resistant to hepatic metabolism, but can result in hepatoxicity.

  26. Synthetic Androgens Danazol : It is a weak androgen, derivative of testosterone which has anti-estrogenic activity. • Primarily used in endometriosis and fibrocystic breast disease. • It is also used in the treatment of hereditary angioedema (↑C-1 esterase inhibitor).

  27. Synthetic androgens

  28. Androgens Clinical uses : • Hypogonadism. • Endometriosis. • Anemia. • Osteoporosis. • Aging.

  29. Androgens Adverse effects : • Hirsutism, acne, deepening of voice. • Cholestatic jaundice. Contraindications : • Pregnancy. • Prostate cancer.

  30. Anti-androgens There are different types of anti-androgens • Androgen receptor antagonist • GnRH analogs • Androgen synthesis inhibitors Ketoconazole

  31. Anti-androgens

  32. Anti-Androgens GnRH agonist • GnRH agonists initially ↑ FSH and LH secretion "flare effect". However, after about two weeks, a profound hypogonadal effect is achieved through receptor down regulation. • Goserelin Zoladex, Buserelin • Used for prostate cancer and male baldness

  33. Anti-androgens Finasteride : • Orally active and inhibits 5-α-reductase -IIenzyme producing a reduction of dihydrotestosterone in prostate and skin. • Dihydrotestosterone is an important androgen in the prostate. • It is approved for treatment of benign hypertrophy of prostate.

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